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Restrict the search for
beta carotene
to a specific field?
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Lorediplon is a novel non-benzodiazepine, the hypnotic drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep. As compared with other selective benzodiazepine receptor agonists, lorediplon has demonstrated in pre-clinical studies a potent hypnotic profile with potential advantages in sleep maintenance and sleep architecture preservation associated with a good safety profile, that is, no induction of tolerance, lack of next-day hangover effect, weak effect on muscular tone, and weak interaction with ethanol. Lorediplon demonstrated a minimum of 10-fold and the 6-fold increase in potency (respectively) in the spontaneous motor activation studies, compared with the currently marketed hypnotics (zolpidem and zaleplon). Additionally, when the electroencephalogram (EEG) effects of lorediplon and zolpidem were compared in the sleep-wake cycle in the mouse, lorediplon demonstrated a 10-fold increase in potency compared with zolpidem in the sleep-wake cycle and 13% greater possibility of fewer wake episodes than zolpidem. At concentrations of 1.2mg/kg, lorediplon demonstrated a 57%increased effect on Slow Wave Sleep (SWS), when compared with a placebo. In clinical trials, the clinical safety and tolerability were excellent for all doses tested. In pharmacokinetic studies, after oral administration, lorediplon is rapidly absorbed from the gastrointestinal tract reaching maximum plasma concentrations at approximately 2 h. Lorediplon demonstrated a dose-dependent improvement in sleep, whereas zolpidem showed a more sustained wake after sleep onset effect. No next-day hangover effects were observed. These sleep effects are also consistent with the pharmacokinetic profile of lorediplon.
Status:
Investigational
Source:
NCT01348919: Phase 1/Phase 2 Interventional Completed Multiple Myeloma
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Delanzomib (CEP-18770), a proteasome inhibitor, was being developed by Cepahlon (a subsidiary of Teva) for the treatment of cancer and immunological disorders. Delanzomib (CEP-18770) induces apoptotic cell death in multiple myeloma (MM) cell lines and in primary purified CD138-positive explant cultures from untreated and bortezomib-treated MM patients. In vitro, Delanzomib (CEP-18770) has a strong antiangiogenic activity and potently represses RANKL-induced osteoclastogenesis. Delanzomib represses the proteasomal degradation of a variety of proteins, including inhibitory kappaBalpha (IkappaBalpha), resulting in the cytoplasmic sequestration of the transcription factor NF-kappaB; inhibition of NF-kappaB nuclear translocation and transcriptional up-regulation of a variety of cell growth-promoting factors; and apoptotic cell death in susceptible tumor cell populations. In vitro studies indicate that this agent exhibits a favorable cytotoxicity profile toward normal human epithelial cells, bone marrow progenitors, and bone marrow-derived stromal cells relative to the proteasome inhibitor bortezomib. Delanzomib has been in phase II clinical trials for the treatment of multiple myeloma (MM). However, this research has been discontinued. Currently Delanzomib is on Phase I clinical trial for Non-Hodgkin's lymphoma and Solid tumours.
Status:
Investigational
Source:
NCT02205892: Not Applicable Interventional Completed Acne
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Lupeol, a biologically active dietary triterpenoid, is found in many medicinal plants and different fruits such as olives, mangos, and strawberries. Lupeol exhibits a wide spectrum of pharmacological properties including anti-inflammatory, anti-cancer, anti-diabetic, anti-microbial, cardioprotective, and hepatoprotective activities. Lupeol inhibits LPS-induced microglial neuroinflammation via the P38-MAPK and JNK pathways and has therapeutic potential to treat various neuroinflammatory disorders. Lupeol possesses antiskin tumor-promoting effects in CD-1 mouse and inhibits conventional as well as novel biomarkers of tumor promotion. It strongly suppressed lipogenesis by modulating the IGF-1R/phosphatidylinositide 3 kinase (PI3K)/Akt/sterol response element-binding protein-1 (SREBP-1) signaling pathway in SEB-1 sebocytes, and reduced inflammation by suppressing the NF-κB pathway in SEB-1 sebocytes and HaCaT keratinocytes. Lupeol exhibited a marginal effect on cell viability and may have modulated dyskeratosis of the epidermis. These results demonstrate the clinical feasibility of applying lupeol for the treatment of acne.
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Epinine or deoxyepinephrine is an active form of Ibopamine, which is used as a cardiovascular agent in congestive heart failure. Epinine is a stimulant of alpha-adrenoceptor activities: alpha-1 and alpha-2. Experiments on pig’s eyes have shown that epinine can be a promising candidate substance for intraoperative (e.g., cataract surgery) intracameral use in humans.
Status:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Locicortolone is an anti-inflammatory and antiallergic synthetic glucocorticoid. It has high glucocorticoid cytoplasmic receptor binding affinity in vitro (more than four times higher than dexamethasone) but comparable to dexamethasone relative TAT (tyrosine aminotransferase induction) activity. It has six times lower binding affinity to mineralocorticoid receptor in comparison to dexamethasone.
Status:
Investigational
Source:
NCT01039701: Phase 2 Interventional Completed Mild to Moderate Alzheimer's Disease
(2009)
Source URL:
Class (Stereo):
CHEMICAL (UNKNOWN)
Status:
Investigational
Source:
NCT00874302: Phase 3 Interventional Withdrawn Uterine Fibroids
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Telapristone is an orally available 21-substituted-19-nor-progestin and selective progesterone receptor modulator (SPRM), with potential anti-progesterone and antineoplastic activities. Its acetate form, the telapristone Acetate is a clinically used and a studied drug.
Status:
Investigational
Source:
J Anim Physiol Anim Nutr (Berl). Jun 2016;100(3):520-5.: Not Applicable Veterinary clinical trial Completed N/A
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Among the naturally occurring trichothecenes in food and feed, T-2 toxin is a cytotoxic fungal secondary metabolite produced by various species of Fusarium. Following ingestion, T-2 toxin causes acute and chronic toxicity and induces apoptosis in the immune system and fetal tissues. T-2 toxin is usually metabolized and eliminated after ingestion, yielding more than 20 metabolites. Consequently, there is a possibility of human consumption of animal products contaminated with T-2 toxin and its metabolites. The molecular mechanism of inhibition of protein synthesis may be the high affinity of T-2 toxin for the 60S ribosomal subunit.
Status:
Investigational
Source:
NCT00960557: Phase 1 Interventional Completed Neoplasm Metastasis
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Oxi0-4503 (now known as combretastatin A1 phosphate), a diphosphate prodrug of combretastatin A1, was developed by Mateon therapeutics as a second-generation, dual-mechanism vascular disrupting agent from the combretastatin family. On November 21, 2012, Oxi-4503 has been granted orphan designation by the US Food and Drug Administration for the treatment of acute myelogenous leukemia. It is known that the orphan drug designation qualifies a company for several benefits, including the potential for market exclusivity, development grants, and tax credits. Oxi0-4503 is currently participating in phase I/II clinical trial the treatment of patients with acute myelogenous leukemia or myelodysplastic syndrome. In addition, phase I clinical trial was successfully completed where was studied the safety of Oxi0-4503 in patients with advanced solid tumors.
Status:
Investigational
Source:
NCT00274716: Phase 2 Interventional Completed Hypertension
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
